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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-Akt-Ipatasertib
Ipatasertib

Chemical Structure : Ipatasertib

CAS No.: 1001264-89-6

Ipatasertib (GDC-0068, RG7440)

货号: PC-49017Not For Human Use, Lab Use Only.

Ipatasertib (GDC-0068) is a potent, selective, orally bioavailable pan-Akt inhibitor with IC50 values of 5 nM, 18 nM, and 8 nM for Akt1, Akt2, and Akt3, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Ipatasertib (GDC-0068, RG7440) is a potent, selective, orally bioavailable pan-Akt inhibitor with IC50 values of 5 nM, 18 nM, and 8 nM for Akt1, Akt2, and Akt3, respectively.
GDC-0068 blocked Akt signaling both in cultured human cancer cell lines and in tumor xenograft models as evidenced by dose-dependent decrease in phosphorylation of downstream targets.
GDC-0068 blocks cell-cycle progression and reduced viability of cancer cell lines.
Oral administration of GDC-0068 resulted in antitumor activity ranging from tumor growth delay to regression in multiple tumor xenograft models.

物理化学性质&存储条件

分子量 458.003
分子式 C24H32ClN5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S)-(4-chlorophenyl)-1-[4-[(5R,7R)-6,7-dihydro-7-hydroxy-5-methyl-5H-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-1-propanone

参考文献

1. Blake JF, et al. J Med Chem. 2012 Sep 27;55(18):8110-27.

2. Lin J, et al. Clin Cancer Res. 2013 Apr 1;19(7):1760-72.

3. Zhai B, et al. Mol Cancer Ther. 2014 Jun;13(6):1589-98.

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